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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
22
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pubmed:dateCreated |
2010-10-19
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pubmed:abstractText |
A novel ?-tryptase inhibitor with a basic benzylamine P1 group, a piperidine-amide linker, and a substituted indole P4 group was discovered. A substitution at 4-indole position was introduced to constrain the conformational flexibility of the inhibitor to the bioactive conformation exhibited by X-ray structures so that entropic penalty was decreased. More importantly, this constrained conformation limited the accessibility of this molecule to anti-targets, especially SSAO, so that an enhanced metabolic profile was achieved.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:CairnsJenniferJ,
pubmed-author:ChenXinX,
pubmed-author:Choi-SledeskiYong MiYM,
pubmed-author:LiangGuyanG,
pubmed-author:MinnichAnneA,
pubmed-author:NieduzakThaddeusT,
pubmed-author:PoliGregoryG,
pubmed-author:ShumPatrickP,
pubmed-author:SidesKeithK,
pubmed-author:StoklosaGregoryG,
pubmed-author:TsayJosephJ,
pubmed-author:VazRoy JRJ,
pubmed-author:WangJieJ,
pubmed-author:WangQingpingQ,
pubmed-author:ZhaoZhichengZ
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pubmed:copyrightInfo |
Copyright © 2010 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
20
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
6721-4
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pubmed:meshHeading |
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pubmed:year |
2010
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pubmed:articleTitle |
A conformationally constrained inhibitor with an enhanced potency for ?-tryptase and stability against semicarbazide-sensitive amine oxidase (SSAO).
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pubmed:affiliation |
Drug Design, Chemical and Analytical Science, Sanofi-Aventis Pharmaceuticals, Route 202-206, Bridgewater, NJ 08807, USA. guyan.liang@sanofi-aventis.com
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pubmed:publicationType |
Journal Article
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